KY-02327 是 KY-02061的一种类似物,具有代谢稳定性。KY-02327是Dishevelled (Dvl)-CXXC5相互作用抑制剂。KY-02327激活Wnt/β-CATenin 途径,从而促进成骨细胞分化。
产品描述
KY-02327 is a metabolically stabilized KY-02061 analog. KY-02327 is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation.
体外活性
KY-02327 (1-10 μM; 2 days; MC3T3E1 cells, a murine pre-osteoblast cell line) increases β-catenin protein level together with Runx2 and accumulated nuclear β-catenin in a dose-dependent manner [1]. KY-02327 (1-10 μM) increases the mRNA levels of collagen 1a ( Col1a ) and osteocalcin ( OCN ) which are the osteoblast differentiation markers[1].
体内活性
KY-02327 (20 mg/kg; p.o.; 5 sequential days per week for 4 weeks) successfully rescues bone loss in the ovariectomized (OVX) mouse model which is potential candidate for the development of bone anabolic anti-osteoporosis drug[1] . Animal Model: 8-week-old female BL6 mice (ovariectomized (OVX)-induced osteoporosis model mice) [1] Dosage: 20 mg/kg Administration: P.o.; administered for 5 sequential days per week for 4 weeks Result: Newly formed bones which labeled with calcein were decreased in the femur of vehicle‐ reated OVX mice.
Cas No.
2093407-25-9
分子式
C20H27N3O4
分子量
373.453
储存和溶解度
DMSO:100 mg/mL (267.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years